Effective suppression of luteinizing hormone and testosterone by single doses of the new gonadotropin-releasing hormone antagonist cetrorelix (SB-75) in normal men.

Behre HM, Klein B, Steinmeyer E, McGregor GP, Voigt K, Nieschlag E

The Journal of clinical endocrinology and metabolism1 Aug 1992Cited by 33 (Europe PMC)

PMID1639941DOI10.1210/jcem.75.2.1639941PepBankPUB-01639941

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Summary

The text of this summary is not shown here, because the article license does not allow reuse. Read it at the source (opens in a new tab)

Text rights: Publisher copyright. Results still quote short attributed sentences.

Results from this study14

14 results from studies that gave the peptide. 14 results from people.

01HumanRandomized controlled trialEfficacy outcome
In normal men, cetrorelix suppressed LH dose- and time-dependently, with maximal suppression 4-6 h after injection.
In plain wordsIn normal men, cetrorelix reduced LH most strongly 4-6 h after injection.
Peptide
Cetrorelix
Outcome
DecreaseLH secretion
Study
n = 30
Outcome group
Sex hormones and fertility · Endocrine and hormones
Studied dose
0.25, 0.5, 1.0, 2.0 and 5.0 mg · subcutaneous · single doseAs given in this study (human).
Measurements
Time of maximal LH suppression
4 to 6 h
after injection
Source sentences
Summary
LH secretion was suppressed dose- and time-dependently; maximal suppression occurred 4-6 h postinjection.
2 context sentences(design, population, supporting numbers)
Summary · context
A clinical phase I study was performed to assess the hormonal effects of this highly potent antagonist in normal men.
Summary · context
After 2 control examinations 30 young male volunteers were randomly assigned to 6 treatment groups (n = 5/group), and single doses of 0 (placebo), 0.25, 0.5, 1.0, 2.0, and 5.0 mg cetrorelix were administered sc.
Report a problemFND-0163994103
02HumanRandomized controlled trialEfficacy outcome
In normal men, cetrorelix 1.0 mg reduced testosterone at 8 h to 7.5 +/- 1.1 versus placebo's 15.8 +/- 2.2 nmol/L.
In plain wordsIn normal men, cetrorelix 1.0 mg reduced testosterone more than placebo at 8 h.
Peptide
Cetrorelix
Outcome
DecreaseMaximal testosterone suppression
Study
n = 10
Comparator
Placebo
Outcome group
Sex hormones and fertility · Endocrine and hormones
Studied dose
1.0 mg · subcutaneous · single doseAs given in this study (human).
Measurements
Testosterone at maximal suppression (8 h), 1.0 mg
7.5 nmol/L
1.0 mg cetrorelix group; +/- 1.1
Testosterone at 8 h, placebo
15.8 nmol/L
placebo group; +/- 2.2
Source sentences
Summary
After the administration of 1.0 mg cetrorelix, maximal suppression was seen 8 h after injection, with testosterone levels of 7.5 +/- 1.1 nmol/L compared to 15.8 +/- 2.2 nmol/L in the placebo group.
3 context sentences(design, population, supporting numbers)
Summary · context
Doses of 1.0, 2.0, and 5.0 mg cetrorelix significantly suppressed testosterone secretion compared to that in the placebo group.
Summary · context
A clinical phase I study was performed to assess the hormonal effects of this highly potent antagonist in normal men.
Summary · context
After 2 control examinations 30 young male volunteers were randomly assigned to 6 treatment groups (n = 5/group), and single doses of 0 (placebo), 0.25, 0.5, 1.0, 2.0, and 5.0 mg cetrorelix were administered sc.
Report a problemFND-0163994105
03HumanRandomized controlled trialEfficacy outcome
In normal men, cetrorelix 2.0 mg reduced testosterone at 12 h to 4.9 +/- 0.5 versus placebo's 16.5 +/- 1.7 nmol/L.
In plain wordsIn normal men, cetrorelix 2.0 mg reduced testosterone more than placebo at 12 h.
Peptide
Cetrorelix
Outcome
DecreaseMaximal testosterone suppression
Study
n = 10
Comparator
Placebo
Outcome group
Sex hormones and fertility · Endocrine and hormones
Studied dose
2.0 mg · subcutaneous · single doseAs given in this study (human).
Measurements
Testosterone at maximal suppression (12 h), 2.0 mg
4.9 nmol/L
2.0 mg cetrorelix group; +/- 0.5
Testosterone at 12 h, placebo
16.5 nmol/L
placebo group; +/- 1.7
Source sentences
Summary
Maximal testosterone suppression by 2.0 and 5.0 mg cetrorelix occurred 12 h after injection, with testosterone concentrations of 4.9 +/- 0.5 and 2.2 +/- 0.4 nmol/L, respectively, compared to 16.5 +/- 1.7 nmol/L in the placebo group.
3 context sentences(design, population, supporting numbers)
Summary · context
Doses of 1.0, 2.0, and 5.0 mg cetrorelix significantly suppressed testosterone secretion compared to that in the placebo group.
Summary · context
A clinical phase I study was performed to assess the hormonal effects of this highly potent antagonist in normal men.
Summary · context
After 2 control examinations 30 young male volunteers were randomly assigned to 6 treatment groups (n = 5/group), and single doses of 0 (placebo), 0.25, 0.5, 1.0, 2.0, and 5.0 mg cetrorelix were administered sc.
Report a problemFND-0163994106
04HumanRandomized controlled trialEfficacy outcome
In normal men, cetrorelix 5.0 mg reduced testosterone at 12 h to 2.2 +/- 0.4 versus placebo's 16.5 +/- 1.7 nmol/L.
In plain wordsIn normal men, cetrorelix 5.0 mg reduced testosterone more than placebo at 12 h.
Peptide
Cetrorelix
Outcome
DecreaseMaximal testosterone suppression
Study
n = 10
Comparator
Placebo
Outcome group
Sex hormones and fertility · Endocrine and hormones
Studied dose
5.0 mg · subcutaneous · single doseAs given in this study (human).
Measurements
Testosterone at maximal suppression (12 h), 5.0 mg
2.2 nmol/L
5.0 mg cetrorelix group; +/- 0.4
Testosterone at 12 h, placebo
16.5 nmol/L
placebo group; +/- 1.7
Source sentences
Summary
Maximal testosterone suppression by 2.0 and 5.0 mg cetrorelix occurred 12 h after injection, with testosterone concentrations of 4.9 +/- 0.5 and 2.2 +/- 0.4 nmol/L, respectively, compared to 16.5 +/- 1.7 nmol/L in the placebo group.
3 context sentences(design, population, supporting numbers)
Summary · context
Doses of 1.0, 2.0, and 5.0 mg cetrorelix significantly suppressed testosterone secretion compared to that in the placebo group.
Summary · context
A clinical phase I study was performed to assess the hormonal effects of this highly potent antagonist in normal men.
Summary · context
After 2 control examinations 30 young male volunteers were randomly assigned to 6 treatment groups (n = 5/group), and single doses of 0 (placebo), 0.25, 0.5, 1.0, 2.0, and 5.0 mg cetrorelix were administered sc.
Report a problemFND-0163994107
05HumanRandomized controlled trialEfficacy outcome
In normal men, testosterone 24 hours after cetrorelix 1.0 mg no longer differed significantly from placebo.
In plain wordsIn normal men, testosterone 24 hours after cetrorelix 1.0 mg no longer differed significantly from placebo.
Peptide
Cetrorelix
Outcome
No significant changeTestosterone at 24 hours
Study
n = 10
Comparator
Placebo
Outcome group
Sex hormones and fertility · Endocrine and hormones
Studied dose
1.0 mg · subcutaneous · single doseAs given in this study (human).
Source sentences
Summary
Twenty-four hours after the injection of 1.0 and 2.0 mg cetrorelix, testosterone values were no longer significantly different from those in the placebo group, whereas in the 5.0-mg dose group testosterone concentrations increased slightly and reached serum concentrations in the lower normal range after 48 h.
2 context sentences(design, population, supporting numbers)
Summary · context
A clinical phase I study was performed to assess the hormonal effects of this highly potent antagonist in normal men.
Summary · context
After 2 control examinations 30 young male volunteers were randomly assigned to 6 treatment groups (n = 5/group), and single doses of 0 (placebo), 0.25, 0.5, 1.0, 2.0, and 5.0 mg cetrorelix were administered sc.
Report a problemFND-0163994108
06HumanRandomized controlled trialEfficacy outcome
In normal men, testosterone 24 hours after cetrorelix 2.0 mg no longer differed significantly from placebo.
In plain wordsIn normal men, testosterone 24 hours after cetrorelix 2.0 mg no longer differed significantly from placebo.
Peptide
Cetrorelix
Outcome
No significant changeTestosterone at 24 hours
Study
n = 10
Comparator
Placebo
Outcome group
Sex hormones and fertility · Endocrine and hormones
Studied dose
2.0 mg · subcutaneous · single doseAs given in this study (human).
Source sentences
Summary
Twenty-four hours after the injection of 1.0 and 2.0 mg cetrorelix, testosterone values were no longer significantly different from those in the placebo group, whereas in the 5.0-mg dose group testosterone concentrations increased slightly and reached serum concentrations in the lower normal range after 48 h.
2 context sentences(design, population, supporting numbers)
Summary · context
A clinical phase I study was performed to assess the hormonal effects of this highly potent antagonist in normal men.
Summary · context
After 2 control examinations 30 young male volunteers were randomly assigned to 6 treatment groups (n = 5/group), and single doses of 0 (placebo), 0.25, 0.5, 1.0, 2.0, and 5.0 mg cetrorelix were administered sc.
Report a problemFND-0163994109
07HumanNon-randomized trialEfficacy outcome
In normal men, cetrorelix did not significantly suppress FSH.
In plain wordsIn normal men, cetrorelix did not significantly suppress FSH.
Peptide
Cetrorelix
Outcome
No significant changeFSH secretion
Study
n = 30
Outcome group
Sex hormones and fertility · Endocrine and hormones
Studied dose
0.25, 0.5, 1.0, 2.0 and 5.0 mg · subcutaneous · single doseAs given in this study (human).
Source sentences
Summary
Suppression of FSH did not reach statistical significance.
2 context sentences(design, population, supporting numbers)
Summary · context
A clinical phase I study was performed to assess the hormonal effects of this highly potent antagonist in normal men.
Summary · context
After 2 control examinations 30 young male volunteers were randomly assigned to 6 treatment groups (n = 5/group), and single doses of 0 (placebo), 0.25, 0.5, 1.0, 2.0, and 5.0 mg cetrorelix were administered sc.
Report a problemFND-0163994104
08HumanNon-randomized trialSafety outcome
In normal men, transient local erythema at the injection site, which disappeared within 30 min, was the only side-effect observed after cetrorelix.
In plain wordsIn normal men, the only side-effect seen after cetrorelix was redness at the injection site that disappeared within 30 min.
Peptide
Cetrorelix
Outcome
Not applicableInjection-site erythema
Study
n = 30
Outcome group
Adverse events · Skin and wound
Studied dose
0.25, 0.5, 1.0, 2.0 and 5.0 mg · subcutaneous · single doseAs given in this study (human).
Source sentences
Summary
The only side-effect observed after the administration of cetrorelix was a transient local erythema at the injection site that disappeared within 30 min.
2 context sentences(design, population, supporting numbers)
Summary · context
A clinical phase I study was performed to assess the hormonal effects of this highly potent antagonist in normal men.
Summary · context
After 2 control examinations 30 young male volunteers were randomly assigned to 6 treatment groups (n = 5/group), and single doses of 0 (placebo), 0.25, 0.5, 1.0, 2.0, and 5.0 mg cetrorelix were administered sc.
Report a problemFND-0163994111
09HumanNon-randomized trialSafety outcome
In normal men, no local induration occurred after cetrorelix.
In plain wordsIn normal men, no injection-site hardening occurred after cetrorelix.
Peptide
Cetrorelix
Outcome
Not applicableLocal induration
Study
n = 30
Outcome group
Adverse events · Skin and wound
Studied dose
0.25, 0.5, 1.0, 2.0 and 5.0 mg · subcutaneous · single doseAs given in this study (human).
Source sentences
Summary
No local induration or pruritus, or any adverse systemic side-effect occurred in any volunteer.
2 context sentences(design, population, supporting numbers)
Summary · context
A clinical phase I study was performed to assess the hormonal effects of this highly potent antagonist in normal men.
Summary · context
After 2 control examinations 30 young male volunteers were randomly assigned to 6 treatment groups (n = 5/group), and single doses of 0 (placebo), 0.25, 0.5, 1.0, 2.0, and 5.0 mg cetrorelix were administered sc.
Report a problemFND-0163994112
10HumanNon-randomized trialSafety outcome
In normal men, no pruritus occurred after cetrorelix.
In plain wordsIn normal men, no itching occurred after cetrorelix.
Peptide
Cetrorelix
Outcome
Not applicablePruritus
Study
n = 30
Outcome group
Adverse events · Skin and wound
Studied dose
0.25, 0.5, 1.0, 2.0 and 5.0 mg · subcutaneous · single doseAs given in this study (human).
Source sentences
Summary
No local induration or pruritus, or any adverse systemic side-effect occurred in any volunteer.
2 context sentences(design, population, supporting numbers)
Summary · context
A clinical phase I study was performed to assess the hormonal effects of this highly potent antagonist in normal men.
Summary · context
After 2 control examinations 30 young male volunteers were randomly assigned to 6 treatment groups (n = 5/group), and single doses of 0 (placebo), 0.25, 0.5, 1.0, 2.0, and 5.0 mg cetrorelix were administered sc.
Report a problemFND-0163994113
11HumanNon-randomized trialSafety outcome
In normal men, no systemic adverse effects occurred after cetrorelix.
In plain wordsIn normal men, no systemic adverse effects occurred after cetrorelix.
Peptide
Cetrorelix
Outcome
Not applicableSystemic adverse effects
Study
n = 30
Outcome group
Adverse events · Whole body
Studied dose
0.25, 0.5, 1.0, 2.0 and 5.0 mg · subcutaneous · single doseAs given in this study (human).
Source sentences
Summary
No local induration or pruritus, or any adverse systemic side-effect occurred in any volunteer.
2 context sentences(design, population, supporting numbers)
Summary · context
A clinical phase I study was performed to assess the hormonal effects of this highly potent antagonist in normal men.
Summary · context
After 2 control examinations 30 young male volunteers were randomly assigned to 6 treatment groups (n = 5/group), and single doses of 0 (placebo), 0.25, 0.5, 1.0, 2.0, and 5.0 mg cetrorelix were administered sc.
Report a problemFND-0163994114
12HumanNon-randomized trialEfficacy outcome
In normal men, testosterone increased slightly after cetrorelix 5.0 mg and reached the lower normal range after 48 h.
In plain wordsIn normal men, testosterone recovered to the lower normal range 48 h after cetrorelix 5.0 mg.
Peptide
Cetrorelix
Outcome
IncreaseTestosterone recovery
Study
n = 5
Outcome group
Sex hormones and fertility · Endocrine and hormones
Studied dose
5.0 mg · subcutaneous · single doseAs given in this study (human).
Source sentences
Summary
Twenty-four hours after the injection of 1.0 and 2.0 mg cetrorelix, testosterone values were no longer significantly different from those in the placebo group, whereas in the 5.0-mg dose group testosterone concentrations increased slightly and reached serum concentrations in the lower normal range after 48 h.
2 context sentences(design, population, supporting numbers)
Summary · context
A clinical phase I study was performed to assess the hormonal effects of this highly potent antagonist in normal men.
Summary · context
After 2 control examinations 30 young male volunteers were randomly assigned to 6 treatment groups (n = 5/group), and single doses of 0 (placebo), 0.25, 0.5, 1.0, 2.0, and 5.0 mg cetrorelix were administered sc.
Report a problemFND-0163994110
13HumanNon-randomized trialPharmacokinetics
In normal men, cetrorelix reached maximal serum concentrations 1 h after injection.
In plain wordsIn normal men, cetrorelix reached its highest serum concentration 1 h after injection.
Peptide
Cetrorelix
Outcome
Not applicableTime to maximal serum concentration
Study
n: not reported in source
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
0.25, 0.5, 1.0, 2.0 and 5.0 mg · subcutaneous · single doseAs given in this study (human).
Measurements
Time to maximal serum concentration
1 h
after single subcutaneous injection
Source sentences
Summary
After maximal cetrorelix serum levels were achieved 1 h postinjection, the GnRH antagonist serum levels decreased with a terminal t1/2 of 29.8 +/- 4.2 h (mean +/- SE).
2 context sentences(design, population, supporting numbers)
Summary · context
A clinical phase I study was performed to assess the hormonal effects of this highly potent antagonist in normal men.
Summary · context
After 2 control examinations 30 young male volunteers were randomly assigned to 6 treatment groups (n = 5/group), and single doses of 0 (placebo), 0.25, 0.5, 1.0, 2.0, and 5.0 mg cetrorelix were administered sc.
Report a problemFND-0163994101
14HumanNon-randomized trialPharmacokinetics
In normal men, cetrorelix had a terminal half-life of 29.8 +/- 4.2 h.
In plain wordsIn normal men, cetrorelix had a terminal half-life of 29.8 +/- 4.2 h.
Peptide
Cetrorelix
Outcome
Not applicableTerminal half-life
Study
n: not reported in source
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
0.25, 0.5, 1.0, 2.0 and 5.0 mg · subcutaneous · single doseAs given in this study (human).
Measurements
Terminal half-life (mean)
29.8 h
after single subcutaneous injection
Terminal half-life (SE)
4.2 h
standard error of the terminal half-life
Source sentences
Summary
After maximal cetrorelix serum levels were achieved 1 h postinjection, the GnRH antagonist serum levels decreased with a terminal t1/2 of 29.8 +/- 4.2 h (mean +/- SE).
2 context sentences(design, population, supporting numbers)
Summary · context
A clinical phase I study was performed to assess the hormonal effects of this highly potent antagonist in normal men.
Summary · context
After 2 control examinations 30 young male volunteers were randomly assigned to 6 treatment groups (n = 5/group), and single doses of 0 (placebo), 0.25, 0.5, 1.0, 2.0, and 5.0 mg cetrorelix were administered sc.
Report a problemFND-0163994102

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PepBank keeps every version of the data on this study. Status changes from Retraction Watch, Europe PMC and Crossref are listed with their source.

Version 2Current
28 Oct 2026, 02:03 UTC
Study results updated
Version 1
27 Oct 2026, 16:35 UTC
First added · source update from Europe PMC

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